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关于此项目
经验公式(希尔记法):
C13H16N2O · HCl
化学文摘社编号:
分子量:
252.74
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Quality level:
InChI
1S/C13H16N2O.ClH/c1-2-13(12-14-7-8-15-12)9-10-5-3-4-6-11(10)16-13;/h3-6H,2,7-9H2,1H3,(H,14,15);1H
SMILES string
Cl.CCC1(Cc2ccccc2O1)C3=NCCN3
InChI key
DWOIUCRHVWIHAH-UHFFFAOYSA-N
assay
≥98% (HPLC)
solubility
H2O: >20 mg/mL
Quality Level
Gene Information
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
Biochem/physiol Actions
(+)-Isomer is a selective α-adrenoceptor antagonist; (−)-isomer is an imidazoline ligand that induces insulin secretion, mediated by the blockade of ATP-sensitive potassium channels in pancreatic β cells; I1 imidazoline binding site antagonist.
(+)-Isomer is a selective α-adrenoceptor antagonist; (−)-isomer is an imidazoline ligand; I1 imidazoline binding site antagonist.
Features and Benefits
This compound is featured on the Imidazoline Binding Sites and Potassium Channels pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
法规信息
新产品
此项目有
M A Carlisle et al.
The Journal of pharmacology and experimental therapeutics, 274(2), 598-601 (1995-08-01)
I1-imidazoline receptor activation by moxonidine has potent antigastric secretory and gastroprotective effects in rats. We therefore tested whether an imidazoline receptor antagonist, efaroxan, would influence gastric secretion and block the antisecretory and antiulcer effects of moxonidine. When given intracerebroventricularly (i.c.v.)
J C Chapman et al.
Diabetes, 48(12), 2349-2357 (1999-12-02)
The properties of ATP-sensitive K+ (K(ATP)) channels were explored in the electrofusion-derived, glucose-responsive, insulin-secreting cell line BRIN-BD11 using patch-clamp techniques. In intact cells, K(ATP) channels were inhibited by glucose, the sulfonylurea tolbutamide, and the imidazoline compounds efaroxan and phentolamine. Each
Shaifali Bhalla et al.
Pharmacology, biochemistry, and behavior, 103(3), 550-560 (2012-10-30)
The potentiation of oxycodone antinociception by BMS182874 (endothelin-A (ET(A)) receptor antagonist) and agmatine (imidazoline receptor/α(2)-adrenoceptor agonist) is well-documented. It is also known that imidazoline receptors but not α(2)-adrenoceptors are involved in potentiation of oxycodone antinociception by agmatine and BMS182874 in
Fei Li et al.
Addiction biology, 17(2), 392-408 (2011-10-05)
Agmatine, an endogenous ligand for imidazoline receptor, has been shown to prevent opioid dependence, but not much is known about the mechanisms of the effect of agmatine. In the present study, we investigated the function of I1 imidazoline receptor and
I I Zaitseva et al.
Cellular and molecular life sciences : CMLS, 65(7-8), 1248-1255 (2008-02-19)
An insufficient number of insulin-producing beta-cells is a major cause of defective control of blood glucose in both type 1 and type 2 diabetes. The aim of this study was to clarify whether the insulinotropic imidazolines can affect the survival
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